A New Potent Analgetic Antagonist
نویسندگان
چکیده
منابع مشابه
Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist.
The highly potent vanilloid receptor (VR) agonist resiniferatoxin has been radiolabeled with 125I, and the pharmacology to the cloned rodent VR, VR1, and the endogenous VR in rat spinal cord membranes has been characterized. [125I]RTX binding to human embryonic kidney 293 cells expressing VR1 was reversible and with high affinity (Kd = 4.3 nM) in an apparent monophasic manner. In rat spinal cor...
متن کاملACCELERATED COMMUNICATION Iodo-Resiniferatoxin, a New Potent Vanilloid Receptor Antagonist
The highly potent vanilloid receptor (VR) agonist resiniferatoxin has been radiolabeled with I, and the pharmacology to the cloned rodent VR, VR1, and the endogenous VR in rat spinal cord membranes has been characterized. [I]RTX binding to human embryonic kidney 293 cells expressing VR1 was reversible and with high affinity (Kd 5 4.3 nM) in an apparent monophasic manner. In rat spinal cord memb...
متن کاملN1-dansyl-spermine: a potent polyamine antagonist.
The potential polyamine antagonist action of N1-dansyl-spermine (a potent NMDA antagonist) was assessed in two in vivo mouse models of polyamine action. Co-administration of N1-dansyl-spermine (2-10 microg, i.c.v.) with spermine (100 microg, i.c.v.) resulted in a dose-dependent antagonism of the spermine-induced CNS excitation (body tremor and fatal tonic convulsions). In addition, the same dos...
متن کاملPharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix.
We describe the pharmacological profile in rats and monkeys of degarelix (FE200486), a member of a new class of long-acting gonadotropin-releasing hormone (GnRH) antagonists. At single subcutaneous injections of 0.3 to 10 microg/kg in rats, degarelix produced a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosteron...
متن کاملRupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF).
Rupatadine (UR-12592, 8-chloro-6, 11-dihydro-11-[1-[(5-methyl3-pyridinyl) methyl]-4-piperidinylidene]-5H-benzo[5,6]-cyclohepta[1,2b]pyridine ) is a novel compound that inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors (Ki(app) values against [3H]WEB-2086 binding to rabbit platelet membranes and [3H]-pyrilamine binding to gu...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Nature
سال: 1961
ISSN: 0028-0836,1476-4687
DOI: 10.1038/1921089a0